1. Field of Invention
This invention relates to pyrrolylpiperidines, processes for their preparation and uses as antidepressants.
2. Prior Art
Mental illnesses include psychoses and neuroses. The symptoms requiring treatment include depression, anxiety, agitation and hallucinations. Drugs used particularly for treatment of both reactive and endogenous depressions include monoamine oxidase (MAO) inhibitors such as iproniazide, tranylcypromine, nialamide, phenelzine and pargyline and the non-MAO inhibiting tricyclic aromatic dibenzazepines such as imipramine and dibenzocycloheptadienes such as amitriptyline.
All of these drugs have side effects that limit their usefulness. The MAO inhibitors may cause tremors, insomnia, hyperhydrosis, agitation, hypermaniac behavior, confusion, hallucinations, convulsions, orthostatic hypertension and death. They frequently cause dizziness, vertigo, headache, inhibition of ejaculation, difficulty in urination, weakness, fatigue, dry mouth, constipation and blurred vision. Imipramine may cause blurred vision, dryness of mouth, constipation, urinary retention, orthostatic hypotension, respiration depression, myocardial infarction and congestive heart failure. Similar difficulties are experienced with amitriptyline.
There is a genuine need for psychotherapeutic agents which are effective and have fewer side effects than the drugs in use today. There is also a need for drugs which have different modes of action than the presently used ones since none is completely effective. The compounds of the present invention satisfy these criteria.
Japanese published Appln. No. 73/56687 to Yoshitomi Pharmaceutical Industries, Inc. discloses antidiabetic and antiinflammatory agents including compounds of the formula: ##STR1## where R=H or alkyl. The compounds are prepared by dehydrating the corresponding piperidinols.